公开(公告)号：US20130204006A1

公开(公告)日：2013-08-08

申请号：US13814592

申请日：2010-10-25

申请人： Herve Richard ,  Patricio Guerreiro ,  Jianping Guo ,  Wensheng Tang

发明人： Herve Richard ,  Patricio Guerreiro ,  Jianping Guo ,  Wensheng Tang

IPC分类号： C07F7/08

CPC分类号： C07F7/0879 ,  C07D249/20 ,  C07F7/0838

摘要： A process for preparing a siloxane compound comprising a 2-hydroxyphenyl benzotriazole function which comprises at least one step in which a reaction for hydrosilylation of a compound 2-hydroxyphenyl benzotriazole comprising a substituent having a terminal double bond with a siloxane compound comprising an SiH function is carried out in the presence of a catalyst and of at least one volatile organic solvent corresponding to one of formula (VII) or (VIII). in which R4 and R5, which may be identical or different, represent a linear or branched C1-C4 alkyl radical, with the proviso that the sum of the carbons of R4 and R5 is less than or equal to 6; y is and integer between 1 and 3; R6 which may be identical or different, are linear or branched C1-C3 alkyl radicals, with the proviso that the sum of the carbons of R6 is less than or equal to 6 is disclosed.

摘要翻译： 一种制备包含2-羟基苯基苯并三唑功能的硅氧烷化合物的方法，其包含至少一个步骤，其中包含具有末端双键的取代基的化合物2-羟基苯基苯并三唑与包含SiH官能团的硅氧烷化合物的氢化硅烷化反应是 在催化剂和对应于式（VII）或（VIII）之一的至少一种挥发性有机溶剂的存在下进行。 其中可以相同或不同的R 4和R 5表示直链或支链C 1 -C 4烷基，条件是R 4和R 5的碳的总和小于或等于6; y为1和3之间的整数; 可以相同或不同的R 6是直链或支链C 1 -C 3烷基，条件是R6的碳原子总数小于或等于6。

公开(公告)号：US09206204B2

公开(公告)日：2015-12-08

申请号：US13814592

申请日：2010-10-25

申请人： Herve Richard ,  Patricio Guerreiro ,  Jianping Guo ,  Wensheng Tang

发明人： Herve Richard ,  Patricio Guerreiro ,  Jianping Guo ,  Wensheng Tang

IPC分类号： C07F7/08 ,  C07D249/20

CPC分类号： C07F7/0879 ,  C07D249/20 ,  C07F7/0838

摘要： A process for preparing a siloxane compound comprising a 2-hydroxyphenyl benzotriazole function which comprises at least one step in which a reaction for hydrosilylation of a compound 2-hydroxyphenyl benzotriazole comprising a substituent having a terminal double bond with a siloxane compound comprising an SiH function is carried out in the presence of a catalyst and of at least one volatile organic solvent corresponding to one of formula (VII) or (VIII). in which R4 and R5, which may be identical or different, represent a linear or branched C1-C4 alkyl radical, with the proviso that the sum of the carbons of R4 and R5 is less than or equal to 6; y is and integer between 1 and 3; R6 which may be identical or different, are linear or branched C1-C3 alkyl radicals, with the proviso that the sum of the carbons of R6 is less than or equal to 6 is disclosed.

摘要翻译： 一种制备包含2-羟基苯基苯并三唑功能的硅氧烷化合物的方法，其包含至少一个步骤，其中包含具有末端双键的取代基的化合物2-羟基苯基苯并三唑与包含SiH官能团的硅氧烷化合物的氢化硅烷化反应是 在催化剂和对应于式（VII）或（VIII）之一的至少一种挥发性有机溶剂的存在下进行。 其中可以相同或不同的R 4和R 5表示直链或支链C 1 -C 4烷基，条件是R 4和R 5的碳的总和小于或等于6; y为1和3之间的整数; 可以相同或不同的R 6是直链或支链C 1 -C 3烷基，条件是R6的碳原子总数小于或等于6。

公开(公告)号：US08614337B2

公开(公告)日：2013-12-24

申请号：US13394614

申请日：2010-09-07

申请人： Xungui He ,  Jianping Guo ,  Yanling Wang ,  Wensheng Tang ,  Xingzhong Zhang ,  Xuezhang Wang ,  Yuan Wang

发明人： Xungui He ,  Jianping Guo ,  Yanling Wang ,  Wensheng Tang ,  Xingzhong Zhang ,  Xuezhang Wang ,  Yuan Wang

IPC分类号： C07D333/20 ,  C07D333/22

CPC分类号： C07D333/20 ,  C07B57/00

摘要： The chiral compound S-5-substituted-N-2′-(thienyl-2-yl-)ethyl-tetralin-2-amine or its chiral acid salts and preparation method thereof are disclosed, and the method for preparing Rotigotine by using the chiral compound is also disclosed. Racemic 5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine (compound 1) is resolved by using a conventional chiral acid to obtain an optically pure chiral acid salt of S-5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine, which is then dissociated to obtain S-5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine (compound 2). The compound 2 or chiral acid salt thereof is alkylated and deprotected to produce rotigotine (compound 5).

摘要翻译： 公开了手性化合物S-5-取代-N-2' - （噻吩基-2-基） - 乙基 - 四氢化萘-2-胺或其手性酸盐及其制备方法， 还公开了手性化合物。 通过使用常规的手性酸来拆分外消旋的5-取代的N-2' - （噻吩-2-基）乙基 - 四氢化萘-2-胺（化合物1），得到光学纯的手性酸S-5- 取代的N-2' - （噻吩-2-基）乙基 - 四氢化萘-2-胺，然后将其解离得到S-5-取代的N-2' - （噻吩-2-基） 四氢化萘-2-胺（化合物2）。 将化合物2或其手性酸式盐进行烷基化和脱保护，得到罗替戈汀（化合物5）。

公开(公告)号：US20130046100A1

公开(公告)日：2013-02-21

申请号：US13394614

申请日：2010-09-07

申请人： Xungui He ,  Jianping Guo ,  Yanling Wang ,  Wensheng Tang ,  Xingzhong Zhang ,  Xuezhang Wang ,  Yuan Wang

发明人： Xungui He ,  Jianping Guo ,  Yanling Wang ,  Wensheng Tang ,  Xingzhong Zhang ,  Xuezhang Wang ,  Yuan Wang

IPC分类号： C07D333/20 ,  C07D333/22

CPC分类号： C07D333/20 ,  C07B57/00

摘要： The chiral compound S-5-substituted-N-2′-(thienyl-2-yl-)ethyl-tetralin-2-amine or its chiral acid salts and preparation method thereof are disclosed, and the method for preparing Rotigotine by using the chiral compound is also disclosed. Racemic 5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine (compound 1) is resolved by using a conventional chiral acid to obtain an optically pure chiral acid salt of S-5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine, which is then dissociated to obtain S-5-substituted-N-2′-(thien-2-yl-)ethyl-tetralin-2-amine (compound 2). The compound 2 or chiral acid salt thereof is alkylated and deprotected to produce rotigotine (compound 5).

摘要翻译： 公开了手性化合物S-5-取代-N-2' - （噻吩基-2-基） - 乙基 - 四氢化萘-2-胺或其手性酸盐及其制备方法， 还公开了手性化合物。 通过使用常规的手性酸来拆分外消旋的5-取代的N-2' - （噻吩-2-基）乙基 - 四氢化萘-2-胺（化合物1），得到光学纯的手性酸S-5- 取代的N-2' - （噻吩-2-基）乙基 - 四氢化萘-2-胺，然后将其解离得到S-5-取代的N-2' - （噻吩-2-基） 四氢化萘-2-胺（化合物2）。 将化合物2或其手性酸式盐进行烷基化和脱保护，得到罗替戈汀（化合物5）。